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Preparation of cefepime hydrochloride by sodium salt precipitation method

The technology of cefepime hydrochloride and sodium salt is applied in the field of preparation of cephalosporin compounds, which can solve the problems of increasing impurities, deepening the color of feed liquid, affecting product purity, etc., so as to improve product quality, reduce the amount of hydrochloric acid, Avoid darkening effects

Inactive Publication Date: 2009-11-18
SHENZHEN SALUBRIS PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In actual production, this method exposes cefepime to a weakly alkaline environment for a long time, which will easily lead to the deepening of the color of the feed liquid and the increase of impurities, which will eventually affect the purity of the product

Method used

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  • Preparation of cefepime hydrochloride by sodium salt precipitation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Dissolve 171g of sodium isooctanoate (1.03mol) in 900mL of water and 200mL of acetone at room temperature (15-25°C), and add 300g of cefepime sulfate (0.52mol, weight based on anhydrous substance) in batches under effective stirring to form Good fluidity paste system. After 10 minutes, add 1600 mL of acetone and appropriate amount of activated carbon, and stir for 30 minutes. The solid was isolated by centrifugation or suction filtration. Wash the filter cake with 500 mL of acetone-water 2:1 (v / v) mixed solution, and combine the filtrates. 18% HCl was added to the filtrate with stirring to pH 1.0-1.5. Then 8 L of acetone was added over 1 hour. The temperature of the system was lowered to 5-10° C., and the stirring was continued for 1 hour. Suction. The filter cake was washed with acetone and dried under vacuum at 40° C. to obtain about 270 g of white crystalline powder. The purity is 99.7%, the water content is 3.8% (K-F method), and the residual acetone is 0.25%....

Embodiment 2

[0032] Add 300g of cefepime sulfate (0.52mol, the weight is based on anhydrous matter) to 900mL of water at room temperature (15-25°C), and add about 20% sodium hydroxide aqueous solution dropwise under vigorous stirring until the pH of the system is between 5.5-6.5. between. Then add 2100mL acetone and an appropriate amount of activated carbon, and stir for 30 minutes. The solid was isolated by centrifugation or suction filtration. Wash the filter cake with 500 mL of acetone-water 2:1 (v / v) mixed solution, and combine the filtrates. 30% HCl was added to the filtrate with stirring until pH 1.0-1.5. Then 8 L of acetone was added over 1 hour. The temperature of the system was lowered to 5-10° C., and the stirring was continued for 1 hour. Suction. The filter cake was washed with acetone and dried under vacuum at 40° C. to obtain about 270 g of white crystalline powder. The purity is above 99.7%, the water content is 3-4%, and the residual acetone is less than 0.4%. The pr...

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Abstract

The invention relates to a method for preparing cefepime hydrochloride. The method is to adjust the cefepime sulfate solution to weakly acidic to neutral with water-soluble alkaline sodium salt (sodium acetate, sodium lactate, sodium isooctanoate, sodium carbonate, sodium bicarbonate, sodium hydroxide or any mixture thereof), adding organic The solvent precipitates out the resulting sodium sulfate, sodium bisulfate or their hydrates. Then add hydrochloric acid to form a salt to obtain cefepime hydrochloride. The method effectively avoids the degradation of cefepime, improves the yield and purity of the product; greatly reduces the corrosion of equipment by the acidic feed liquid; obviously reduces the consumption of organic solvents, and improves the production efficiency.

Description

technical field [0001] The invention relates to a preparation method of cephalosporin compounds, in particular to a method for preparing cefepime hydrochloride by using cefepime sulfate as a raw material. Background technique [0002] Cefepime (formula I) is a fourth-generation cephalosporin antibiotic for injection, which has good antibacterial activity against Gram-negative bacteria, Gram-positive bacteria and anaerobic bacteria, and has good antibacterial activity against β-lactamase. Compared with the third-generation cephalosporin antibiotics, it has a wider antibacterial spectrum and antibacterial activity. It is clinically used to treat severe infections. The earliest cefepime document is US Patent 4,406,899. [0003] Cefepime is a thermally unstable and highly water-soluble neutral inner salt, its structure is shown in the figure below. Due to the existence of carboxyl negative ions in pure cefepime, it is easy to combine with protons in aqueous solution, which pr...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D501/46
Inventor 谭端明张志国叶澄海
Owner SHENZHEN SALUBRIS PHARMA CO LTD